Synthesis, in vitro and in vivo cytotoxicity, and prediction of the intestinal absorption of substituted 2-ethoxycarbonyl-imidazo[2,1-b]benzothiazoles was written by Trapani, G.;Franco, M.;Latrofa, A.;Reho, A.;Liso, G.. And the article was included in European Journal of Pharmaceutical Sciences in 2001.Recommanded Product: 5,6-Dimethoxybenzo[d]thiazol-2-amine This article mentions the following:
The imidazobenzothiazole compounds together with an imidazobenzoxazole, and an imidazobenzoimidazole were prepared and their cytotoxic activity evaluated at the National Cancer Institute (NCI) for testing against a panel of approx. 60 tumor cell lines. Four compounds exhibited interesting in vitro cytotoxic activity. The most active imidazobenzothiazole derivative I was further evaluated as a cytotoxic agent in the hollow fiber assay and showed a score greater than the min. values for xenograft testing together with a net cell kill. Comparison with the results displayed in the in vivo assay by standard antitumor drugs in clin. use revealed a significant in vivo activity of the benzothiazole compound COMPARE analyses for 16 of the compounds against the NCI’s standard agent database show poor or no correlation, and it might suggest for these compounds a mechanism of action unrelated to that of any known drug. Furthermore, the benzothiazole I did not show significant antitumor activity in a panel of two xenotransplanted tumors (i.e. colon and non-small cell lung tumors). By computing the polar surface area of the compounds with the MAREA computer program it was established that the most active compounds should experience good intestinal permeability. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6Recommanded Product: 5,6-Dimethoxybenzo[d]thiazol-2-amine).
5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Recommanded Product: 5,6-Dimethoxybenzo[d]thiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica